US2023365639A1PendingUtilityA1

Defensin fragment derived lipopeptides for treatment of drug-resistant microorganisms

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Assignee: AESCULUS BIO APSPriority: Sep 14, 2020Filed: Sep 14, 2021Published: Nov 16, 2023
Est. expirySep 14, 2040(~14.1 yrs left)· nominal 20-yr term from priority
Inventors:Jan WehkampLouis Köninger
C07K 14/4723A61K 47/542A61P 31/00A61K 47/65A61K 47/10A61K 47/26A61K 47/554A61P 31/04A61P 1/00A61P 31/10A61K 38/00Y02A50/30
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PatentIndex Score
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Cited by
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References
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Claims

Abstract

The present invention relates to development of innovative antibiotics against drug resistant bacteria, viruses, protozoa, fungi or worms based on coupling of lipopeptides to fragments of human defensins to achieve high antimicrobial efficacy and biofilm degradation as well as low development of resistance while preserving the natural microbiota thus not only eradicating bacterial, viral, protozoal, fungal or worm infection but preventing a number of disorders associated with antibiotic treatment e.g. infection with C. difficile'.

Claims

exact text as granted — not AI-modified
1 . A compound having the structure a-b-c, wherein a) comprises or is lauric acid, palmitic acid, or cholesterol; b) is an optional linker/spacer selected from sugars and/or amino acids and/or PEG agents and c) is a peptide selected from fragments of human beta defensin-1 (hBD-1). 
     
     
         2 . The compound of  claim 1 , wherein a comprises or is lauric or palmitic acid, preferably palmitic acid. 
     
     
         3 . The compound of  claim 1  or  2 , wherein the fragment of hBD-1 is SEQ ID NO: 36 or 39. 
     
     
         4 . The compound of any of the preceding claims, wherein the compound comprises or consists of the C-terminal eight amino acids of hBD-1 chemically modified with palmitic acid and/or 8-amino-3.6-dioxaoctanoic acid. 
     
     
         5 . The compound of any of the preceding claims, wherein the compound has antimicrobial activity. 
     
     
         6 . The compound of any of the preceding claims, wherein the compound is a modified fragment of human beta defensin-1 (hBD-1), wherein the compound is selected from the list:
 Pam2-Glc-Suc-RGKAKCCK (PAM-1)   Pam-RGKAKCCK (PAM-2),   Pam-Ado-RGKAKCCK (PAM-3),   Pam3Cys-RGKAKCCK (PAM-4), and   Pam-Lys(Pam)-RGKAKCCK (PAM-5).   
     
     
         7 . The compound of any of the preceding claims for use in the treatment of any Gram-positive and/or Gram-negative bacterial infection, viral infections, protozoal infections, fungal infections or worm infections (helminthiasis). 
     
     
         8 . The compound of any of the preceding claims for use in the treatment of any drug resistant Gram-positive and/or Gram-negative bacterial infection. 
     
     
         9 . The compound of any of the preceding claims for use in the treatment of drug resistant viral infections. 
     
     
         10 . The compound of any of the preceding claims for use in the treatment of drug resistant protozoal infections. 
     
     
         11 . The compound of any of the preceding claims for use in the treatment of drug resistant fungal infections. 
     
     
         12 . The compound of any of the preceding claims for use in the treatment of drug resistant worm infections (helminthiasis). 
     
     
         13 . The compound of any of the preceding claims for use in the treatment of any bacterial infection caused by ESKAPE pathogens ( E. faecium; S. aureus; K. pneumoniae; A. baumanii; P. aeruginosa  and/or  Enterobacter ). 
     
     
         14 . The compound of any of the preceding claims for use in the treatment of any Gram-positive and/or Gram-negative bacterial gastrointestinal infection. 
     
     
         15 . The compound of any of the preceding claims for use in the treatment of any drug resistant Gram-positive and/or Gram-negative bacterial gastrointestinal infection. 
     
     
         16 . The compound of any of the preceding claims for use in the treatment of any gastrointestinal infection caused by ESKAPE pathogens ( E. faecium; S. aureus; K. pneumoniae; A. baumanii; P. aeruginosa  and/or  Enterobacter ). 
     
     
         17 . The compound of any of the preceding claims for use in the treatment of any bacterial infection specifically killing the pathogens through biofilm eradication and bacterial membrane disruption while preserving or increasing the microbiota e.g. bacterial abundance, richness and diversity and/or bacterial phylae with minimal development of bacterial resistance. 
     
     
         18 . The compound of any of the preceding claims for use in the treatment of any bacterial, gastrointestinal infection specifically killing the pathogens through biofilm eradication and bacterial membrane disruption while preserving or increasing the microbiota e.g. bacterial abundance, richness and diversity and/or bacterial phylae with minimal development of bacterial resistance. 
     
     
         19 . The compound of any of the preceding claims for use in the treatment of any bacterial infection specifically killing the pathogens while preserving or increasing the microbiota e.g. bacterial gene richness and/or bacterial phylae. 
     
     
         20 . The compound of any of the preceding claims for use in the treatment of any bacterial, gastrointestinal infection killing the pathogens while preserving or increasing the gastrointestinal microbiota e.g. bacterial gene richness and/or bacterial phylae. 
     
     
         21 . The compound of any of the preceding claims for use in the killing of any pathogenic bacteria through biofilm eradication and bacterial membrane disruption. 
     
     
         22 . The compound of any of the preceding claims for use in the killing of any pathogenic, gastrointestinal bacteria through biofilm eradication and bacterial membrane disruption. 
     
     
         23 . The compound of any the preceding claims for use in the treatment of any bacterial, gastrointestinal infection preserving the gastrointestinal microbiota thus decreasing the risk of secondary gastrointestinal infections with e.g.  C. difficile.    
     
     
         24 . The compound of any of the preceding claims for use in the treatment of any bacterial infection caused by  S. aureus; E. coli; C. rodentium; P. aeruginosa; S. typhimurium  and/or  S. enteritidis.    
     
     
         25 . The compound of any of the preceding claims for use in the treatment of any bacterial, gastrointestinal infection caused by  S. aureus; E. coli; C. rodentium; P. aeruginosa S. enteritidis  and/or  S. typhimurium.    
     
     
         26 . The compound of any of the preceding claims for use in the treatment of any bacterial infection caused by  S. aureus.    
     
     
         27 . The compound of any of the preceding claims for use in the treatment of any bacterial, gastrointestinal infection caused by  S. aureus.    
     
     
         28 . The compound of any of the preceding claims for use in the treatment of any bacterial infection caused by  E. coli.    
     
     
         29 . The compound of the preceding claims for use in the treatment of any bacterial, gastrointestinal infection caused by  E. coli.    
     
     
         30 . The compound of any of the preceding claims for use in the treatment of any bacterial infection caused by  C. rodentium.    
     
     
         31 . The compound of any of the preceding claims for use in the treatment of any bacterial, gastrointestinal infection caused by  C. rodentium.    
     
     
         32 . The compound of any of the preceding claims for use in the treatment of any bacterial infection caused by  P. aeruginosa.    
     
     
         33 . The compound of any of the preceding claims for use in the treatment of any bacterial, gastrointestinal infection caused by  P. aeruginosa.    
     
     
         34 . The compound of any of the preceding claims for use in the treatment of any bacterial infection caused by  S. enteritidis.    
     
     
         35 . The compound of any of the preceding claims for use in the treatment of any bacterial, gastrointestinal infection caused by  S. enteritidis.    
     
     
         36 . The compound of any of the preceding claims for use in the treatment of any bacterial infection caused by  S. typhimurium.    
     
     
         37 . The compound of any of the preceding claims for use in the treatment of any bacterial, gastrointestinal infection caused by  S. typhimurium.    
     
     
         38 . The compound of any of the preceding claims for use in the treatment of any fungal infection caused by  C. albicans.    
     
     
         39 . The compound of any of the preceding claims for use in the treatment of any fungal, gastrointestinal infection caused by  C. albicans .

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